
科学技术与工程

中国技术经济学会
阿司匹林包合物微孔渗透泵片制备及释药机制考察
Preparation and Release Mechanism of Aspirin Inclusion Micro-porous Osmotic Pump Tablets
依次采用单因素试验和Box-Behnken设计结合响应面法,以释放度为评价指标,优化了阿司匹林包合物微孔渗透泵片的最佳制备工艺。首先制备β-环糊精阿司匹林包合物,再以醋酸纤维素为包衣材料、聚乙二醇4000为致孔剂制备阿司匹林包合物微孔渗透泵片。体外释放度试验表明,该工艺制备的阿司匹林包合物微孔渗透泵片与市售阿司匹林肠溶片在人工胃液中0~2 h内累积释放率分别为1.5%和1.6%;将释放介质调至pH 6.8后,两种剂型在10 h时的累积释药量无显著差异。此外,该包合物微孔渗透泵片在12 h内呈现零级释放且释放较完全(累积释放率>90%),提示有可能减轻药物对胃黏膜的损伤。
The Box-Behnken experimental design and response surface methodology were employed to optimize the preparation of the aspirin micro-porous osmotic pump tablets. The core of the tablet was prepared with aspirin and β-CD inclusion, then osmotic pump tablets were obtained by coating a layer of cellulose acetate containing PEG 4000 as porogenic agent. The in vitro release test shows that the aspirin inclusion complex microporous osmotic pump tablets prepared by this process has a cumulative release rate of 1.5% and 1.6% within 0~2 h in artificial gastric juice compared to commercially available aspirin enteric coated tablets. After adjusting the release medium to pH 6.8, there is no significant difference in the cumulative drug release between the two formulations at 10 h. And the inclusion complex microporous osmotic pump tablet shows zero order release and complete release within 12 h(cumulative release rate > 90%), indicating the possibility of reducing drug damage to the gastric mucosa.
aspirin / microporous osmotic pump tablet / central composite design / release mechanism
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